(E)-GABAB receptor antagonist 1

Modify Date: 2024-01-23 15:31:35

(E)-GABAB receptor antagonist 1 Structure
(E)-GABAB receptor antagonist 1 structure
Common Name (E)-GABAB receptor antagonist 1
CAS Number 1611483-29-4 Molecular Weight 304.38
Density N/A Boiling Point N/A
Molecular Formula C18H24O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of (E)-GABAB receptor antagonist 1


(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM[1].

 Names

Name (E)-GABAB receptor antagonist 1

 (E)-GABAB receptor antagonist 1 Biological Activity

Description (E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM[1].
Target

GABAB receptor[1]

In Vitro (E)-GABAB receptor antagonist 1 (compound 14) decreases agonist GABA-induced maximal effect of IP3 production in HEK293 cells overexpressing GABAB receptors and Gqi9 proteins without changing the EC50[1].
References

[1]. Chen LH, et al. Discovery of a Negative Allosteric Modulator of GABAB Receptors. ACS Med Chem Lett. 2014 May 27;5(7):742-7.

 Chemical & Physical Properties

Molecular Formula C18H24O4
Molecular Weight 304.38